On October 15, 2021, Hu, Yuanyuan; Hu, Chunfang; Pan, Guangxing; Yu, Congwei; Ansari, Mohammad Fawad; Yadav Bheemanaboina, Rammohan R.; Cheng, Yu; Zhou, Chenghe; Zhang, Jiaheng published an article.Formula: C5H5NOS The title of the article was Novel chalcone-conjugated, multi-flexible end-group coumarin thiazole hybrids as potential antibacterial repressors against methicillin-resistant Staphylococcus aureus. And the article contained the following:
The increasing resistance of methicillin-resistant Staphylococcus aureus (MRSA) to antibiotics has led to a growing effort to design and synthesize novel structural candidates of chalcone-conjugated, multi-flexible end-group coumarin thiazole hybrids with outstanding bacteriostatic potential. Bioactivity screening showed that hybrid 5i, which was modified with methoxybenzene, exerted a significant inhibitory activity against MRSA (MIC = 0.004 mM), which was 6 times better than the anti-MRSA activity of the reference drug norfloxacin (MIC = 0.025 mM). Compound 5i neither conferred apparent resistance onto MRSA strains even after multiple passages nor triggered evident toxicity to human hepatocyte LO2 cells and normal mammalian cells (RAW 264.7). Mol. docking showed that highly active mol. 5i might bind to DNA gyrase by forming stable hydrogen bonds. In addition, mol. electrostatic potential surfaces were developed to explain the high antibacterial activity of the target compounds Furthermore, preliminary mechanism studies suggested that hybrid 5i could disrupt the bacterial membrane of MRSA and insert itself into MRSA DNA to impede its replication, thus possibly becoming a potential antibacterial repressor against MRSA. The experimental process involved the reaction of 2-Acetylthiazole(cas: 24295-03-2).Formula: C5H5NOS
The Article related to staphylococcus methicillin resistance antibacterial chalcone macrophage hepatocyte, antibacterial, chalcone, coumarin, dna, mrsa, thiazole, Microbial, Algal, and Fungal Biochemistry: Other and other aspects.Formula: C5H5NOS
Referemce:
Thiazole | C3H3NS – PubChem,
Thiazole | chemical compound | Britannica